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US4066754A Expired / Lapsed US ⏱️ 0.0 years remaining

Slow release bolus

Assignee: Purina Mills LLC
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Filing: 1976-04-26
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Granted: 1978-01-03
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Expires: 1996-04-26
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Abstract

Abstract A composition for slowly releasing a veterinary medicament in a ruminant animal is described. The composition comprises a water-insoluble and water resistant binder a therapeutically active substance and a critical water-insoluble controlled release agent. The process of the invention includes the steps of adding a solution of a water-insoluble binder dissolved in an organic solvent to a mixture of a therapeutically active substance and a water-insoluble dense filler, stirring the mixture until free flowing granules are formed, drying the granules, blending the dried granules with a lubricant and a water insoluble controlled release agent and compressing the mixture into convenient veterinary dosage forms. When the veterinary composition is orally administered to a ruminant animal it remains in the animal's body for a desired period of time and the therapeutically active substance contained therein is released in a predictable and controllable pattern.

Inventors

  • 👤 Shih-Toon Chou

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-29 21:16
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0053; A61K9/0068; A61K31/00; A61K31/63; A61K31/635; A61K31/65; A61K9/20; A61K9/2004; A61K9/2022; A61K9/2063

Claims Analysis

Total Claims: 33
Claim 1
Independent Claim 115 words
An improved method of preparing a sustained release veterinary bolus for ruminant animals having a therapeutically active substance, filler material, binder and lubricant wherein the improvement comprises forming the binder by combining an effective amount of zein and an organic solvent, mixing the binder with the therapeutically active substance and filler material to granulate the mixture, drying the mixture, adding a lubricant, blending the dried mixture with an effective amount of zein to insure sustained release of the therapeutically active substance and forming a bolus of sufficient density that will remain in a ruminant animal to release the therapeutically active substance for a period of time up to 15 days in a predictable, controllable pattern.
Claim 2
Dependent Claim 115 words
An improved method of preparing a sustained release veterinary bolus for ruminant animals having a therapeutically active substance, filler material, binder and lubricant wherein the improvement comprises forming the binder by combining an effective amount of zein and an organic solvent, mixing the binder with the therapeutically active substance and filler material to granulate the mixture, drying the mixture, adding a lubricant, blending the dried mixture with an effective amount of zein to insure sustained release of the therapeutically active substance and forming a bolus of sufficient density that will remain in a ruminant animal to release the therapeutically active substance for a period of time up to 15 days in a predictable, controllable pattern.
Claim 3
Dependent Claim 20 words
The method of claim 1 wherein about 6 to about 35% by weight of zein is utilized in the bolus.
Claim 4
Dependent Claim 20 words
The method of claim 1 wherein about 5 to about 25% by weight of zein is utilized as a binder.
Claim 5
Dependent Claim 20 words
The method of claim 1 wherein about 1 to 10% by weight of zein is utilized as a disintegrating agent.
Claim 6
Dependent Claim 12 words
The method of claim 1 wherein the therapeutically active substance is sulfamethazine.
Claim 7
Dependent Claim 16 words
The method of claim 1 wherein the bolus has a density of about 1.4 to 5.5.
Claim 8
Dependent Claim 142 words
An improved method of preparing a sustained release veterinary bolus for ruminant animals comprising: forming a binder solution by mixing about 5 to 25% by weight of the bolus of a binder material with an organic solvent, mixing about 1 to about 80% by weight of a therapeutically active substance with about 10 to about 95% by weight of a filler material; combining and mixing the binder solution and mixture of therapeutically active substance and filler material to granulate the mixture; drying the mixture; adding about 0.1 to about 0.5% by weight of a lubricant to the mixture; mixing in about 1 to about 10% by weight of a zein disintegrating agent to the mixture and forming a bolus that can be orally administered to ruminant animals to release the therapeutically active substance for a period of time up to 15 days.
Claim 9
Dependent Claim 142 words
An improved method of preparing a sustained release veterinary bolus for ruminant animals comprising: forming a binder solution by mixing about 5 to 25% by weight of the bolus of a binder material with an organic solvent, mixing about 1 to about 80% by weight of a therapeutically active substance with about 10 to about 95% by weight of a filler material; combining and mixing the binder solution and mixture of therapeutically active substance and filler material to granulate the mixture; drying the mixture; adding about 0.1 to about 0.5% by weight of a lubricant to the mixture; mixing in about 1 to about 10% by weight of a zein disintegrating agent to the mixture and forming a bolus that can be orally administered to ruminant animals to release the therapeutically active substance for a period of time up to 15 days.
Claim 10
Dependent Claim 11 words
The method of claim 7 wherein the binder material is zein.
Claim 11
Dependent Claim 12 words
The method of claim 7 wherein the binder material is ethyl cellulose.
Claim 12
Dependent Claim 30 words
The method of claim 9 wherein a binder solution is formed by mixing about 2 to about 8% by weight of the bolus of ethyl cellulose with an organic solvent.
Claim 13
Dependent Claim 19 words
The method of claim 7 wherein the total amount of zein is about 6 to about 35% by weight.
Claim 14
Dependent Claim 22 words
The method of claim 7 wherein the amount of zein utilized as a binder is about 5 to about 25% by weight.
Claim 15
Dependent Claim 18 words
The method of claim 7 wherein the zein utilized as a disintegrating agent is in the powdery form.
Claim 16
Dependent Claim 26 words
The method of claim 7 wherein the therapeutically active substance is selected from the group consisting of sulfonamides, antibiotics, hormones, vitamins, minerals, anthelmintics and anti-bloat agents.
Claim 17
Dependent Claim 27 words
The method of claim 7 wherein the organic solvent is selected from the group consisting of isopropanol, ethanol, methanol, acetone, furfuryl, tetrahydro furfuryl alcohol and combinations thereof.
Claim 18
Dependent Claim 33 words
The method of claim 7 wherein the filler material is selected from the group consisting of iron powder, ferric oxide, calcium sulfate, portland cement, plaster of paris, talc, magnesium oxychloride and mixtures thereof.
Claim 19
Dependent Claim 24 words
The method of claim 7 wherein the lubricant is selected from the group consisting of magnesium stearate, sodium stearate, calcium stearate and stearic acid.
Claim 20
Dependent Claim 18 words
The method of claim 7 wherein the disintegrating agent is a combination of microcrystalline cellulose and powdery zein.
Claim 21
Dependent Claim 20 words
The method of claim 18 wherein about 0.5 to about 1.5% by weight microcrystalline cellulose is combined with powdery zein.
Claim 22
Dependent Claim 99 words
A solid, sustained release veterinary bolus for ruminant animals comprising (1) from about 1 to about 80% by weight of a therapeutically active substance, (2) from about 10 to about 95% by weight of a filler material, (3) from about 0.1 to about 0.5% by weight of a lubricant and (4) from about 6 to about 35% by weight of zein, said veterinary bolus being characterized by containing a binder comprising about 5 to about 25% by weight of zein of foregoing step 4 and a disintegrating agent comprising from about 1 to about 10% by weight of zein.
Claim 23
Dependent Claim 99 words
A solid, sustained release veterinary bolus for ruminant animals comprising (1) from about 1 to about 80% by weight of a therapeutically active substance, (2) from about 10 to about 95% by weight of a filler material, (3) from about 0.1 to about 0.5% by weight of a lubricant and (4) from about 6 to about 35% by weight of zein, said veterinary bolus being characterized by containing a binder comprising about 5 to about 25% by weight of zein of foregoing step 4 and a disintegrating agent comprising from about 1 to about 10% by weight of zein.
Claim 24
Dependent Claim 30 words
The veterinary bolus of claim 20 wherein the therapeutically active substance is released in ruminant animals for a period of time up to 15 days in a predictable controllable pattern.
Claim 25
Dependent Claim 17 words
The veterinary bolus of claim 20 wherein the density of the bolus is about 1.4 to 5.5.
Claim 26
Dependent Claim 20 words
The veterinary bolus of claim 20 wherein the weight of the bolus is from about 2 to about 40 grams.
Claim 27
Dependent Claim 13 words
The veterinary bolus of claim 20 wherein the therapeutically active substance is sulfamethazine.
Claim 28
Dependent Claim 13 words
The veterinary bolus of claim 20 wherein the therapeutically active substance is sulfathiazole.
Claim 29
Dependent Claim 81 words
A solid sustained release veterinary bolus for ruminant animals comprising a therapeutically active substance, filler material, binder, lubricant and disintegrating agent with an effective amount of zein utilized in said binder and disintegrating agent to provide sustained release of said therapeutically active substance for a period of time up to 15 days in a predictable controllable pattern while simultaneously protecting the essential microorganisms normally responsible for digestive fermentation within said ruminant animal from being adversely affected by said therapeutically active substance.
Claim 30
Dependent Claim 81 words
A solid sustained release veterinary bolus for ruminant animals comprising a therapeutically active substance, filler material, binder, lubricant and disintegrating agent with an effective amount of zein utilized in said binder and disintegrating agent to provide sustained release of said therapeutically active substance for a period of time up to 15 days in a predictable controllable pattern while simultaneously protecting the essential microorganisms normally responsible for digestive fermentation within said ruminant animal from being adversely affected by said therapeutically active substance.
Claim 31
Dependent Claim 19 words
The veterinary bolus of claim 26 wherein the amount of zein is about 6 to about 35% by weight.
Claim 32
Dependent Claim 23 words
The veterinary bolus of claim 26 wherein the amount of zein utilized as a binder is about 5 to about 25% by weight.
Claim 33
Dependent Claim 24 words
The veterinary bolus of claim 26 wherein the amount of zein utilized as a disintegrating agent is about 1 to about 10% by weight.

References Cited (Backward Citations)

US2895880A Cited
US3181998A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1981-01-02 1981-07-04 1982-01-03 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1985-01-02 1985-07-04 1986-01-03 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1989-01-02 1989-07-04 1990-01-03 $7700.00 Window Closed / Lapsed

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